- A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs
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A new synthesis of carboxyterfenadine (4), based on the conversion of a α-halo-alkylarylketone into the corresponding substituted 2-arylalkanoic ester, is described. The enantioselective synthesis of its two bioisosteric tetrazole analogs together with preliminary biological results are reported. Copyright (C) 1999 Elsevier Science S.A.
- Di Giacomo, Barbara,Coletta, Donato,Natalini, Benedetto,Ni, Ming-Hong,Pellicciari, Roberto
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p. 600 - 610
(2007/10/03)
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- Antihistaminic compounds, process for their preparation and pharmaceutical compositions containing them
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The present invention relates to terfenadine derivatives of formula where R?, which is in position 1 or 2 of the tetrazole ring, stands for H, or a linear or branched alkyl group containing from 1 to 6 carbon atoms; R? and R?, different from one another, are selected between H and OH, and their pharmaceutically acceptable salts.
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